STAT1/3-IN-1
Based on 1 Customer Validation
STAT1/3-IN-1 is a potent STAT1/3 inhibitor with potent anti-inflammatory effect. STAT1/3-IN-1 inhibits phosphorylation and nuclear translocation of STAT1/3 to modulate microglial inflammation, reduces LPS (HY-D1056)-induced pro-inflammatory cytokines (NO, IL-1β, IL-6, and TNF-α) and inflammatory mediators (iNOS, COX-2). STAT1/3-IN-1 exhibits low toxicity in mice. STAT1/3-IN-1 can be used for the research of neuroinflammation.
For research use only. We do not sell to patients.
- Purity: 99.23%
- CAS No.: 2958649-56-2
- Formula: C28H25ClN6O5
- Molecular Weight:560.99
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
|
COX-2 |
IL-6 |
iNOS |
STAT3 |
STAT1 |
IL-1β |
TNF-α |
STAT1/3-IN-1 (compound 6k) (1-10 μM, 26 h) inhibits LPS-induced NO production with an IC50 of 4.45 μM, while maintains cell viability in BV-2 cells[1].
STAT1/3-IN-1 (5-10 μM; 8 h) significantly downregulates mRNA expression of pro-inflammatory cytokines (IL-1β, IL-6, TNF-α) and inflammatory mediators (iNOS, COX-2) in LPS-stimulated BV-2 cells[1].
STAT1/3-IN-1 (5-10 μM) reduces LPS-induced IL-6 and TNF-α release in BV-2 cells[1].
STAT1/3-IN-1 (5-10 μM; 26 h) dose-dependently reduces iNOS and COX-2 protein expression in LPS-stimulated BV-2 cells[1].
STAT1/3-IN-1 (5-10 μM; 5 h) inhibits STAT1 and STAT3 phosphorylation and reduces nuclear phosphorylated STAT1 and STAT3 in LPS-stimulated BV-2 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LPS-stimulated BV-2 cells
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Concentration:5, 10 μM
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Incubation Time:8 h (2 h pretreatment + 6 h with LPS)
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Result:Significantly downregulated mRNA expression of IL-1β, IL-6, TNF-α, iNOS and COX-2 in LPS-stimulated BV-2 cells.
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Cell Line:LPS-stimulated BV-2 cells
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Concentration:5, 10 μM
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Incubation Time:26 h (2 h pretreatment + 24 h with LPS)
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Result:Decreased LPS-induced iNOS and COX-2 protein expression in a concentration-dependent manner.
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Cell Line:LPS-stimulated BV-2 cells
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Concentration:5, 10 μM
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Incubation Time:5 h (2 h pretreatment + 3 h with LPS)
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Result:Abrogated LPS-induced phosphorylation of STAT1 and STAT3.
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Cell Line:LPS-stimulated BV-2 cells
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Concentration:10 μM
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Incubation Time:5 h (2 h pretreatment + 3 h with LPS)
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Result:Significantly reduced nuclear presence of phosphorylated STAT1 and STAT3 under LPS stimulation.
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Cell Line:LPS-stimulated BV-2 cells
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Concentration:10 μM
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Incubation Time:5 h (2 h pretreatment + 3 h with LPS)
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Result:Decreased levels of phosphorylated STAT1 and STAT3 in nuclear extracts under LPS stimulation.
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Cell Line:LPS-stimulated BV-2 cells
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Concentration:1, 10 μM
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Incubation Time:26 h (2 h pretreatment + 24 h with LPS)
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Result:Showed no significant cytotoxicity, with cell viability of 88.03% (1 μM) and 86.71% (10 μM) compared to the control group.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male and female KM mice[1]
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Dosage:250 mg/kg
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Administration:i.g.; single dose
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Result:Showed no significant differences in body weight, organ indices, GPT and GOT levels compared to vehicle control.
Showed no significant damage in major organs (heart, liver, spleen, lungs, and kidneys).
Chemical Information
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CAS No. 2958649-56-2
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Appearance Solid
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Molecular Weight 560.99
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Formula C28H25ClN6O5
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Color White to off-white
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SMILES
ClC1=C(N2C=C(C3=CC=CC(NC(C4=CN(C[C@@](OCC[C@H]5C)([H])N5C6=O)C6=C(OC)C4=O)=O)=C3)N=N2)C=CC=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (178.26 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (279 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7826 mL | 8.9128 mL | 17.8256 mL | 44.5641 mL |
| 5 mM | 0.3565 mL | 1.7826 mL | 3.5651 mL | 8.9128 mL | |
| 10 mM | 0.1783 mL | 0.8913 mL | 1.7826 mL | 4.4564 mL | |
| 15 mM | 0.1188 mL | 0.5942 mL | 1.1884 mL | 2.9709 mL | |
| 20 mM | 0.0891 mL | 0.4456 mL | 0.8913 mL | 2.2282 mL | |
| 25 mM | 0.0713 mL | 0.3565 mL | 0.7130 mL | 1.7826 mL | |
| 30 mM | 0.0594 mL | 0.2971 mL | 0.5942 mL | 1.4855 mL | |
| 40 mM | 0.0446 mL | 0.2228 mL | 0.4456 mL | 1.1141 mL | |
| 50 mM | 0.0357 mL | 0.1783 mL | 0.3565 mL | 0.8913 mL | |
| 60 mM | 0.0297 mL | 0.1485 mL | 0.2971 mL | 0.7427 mL | |
| 80 mM | 0.0223 mL | 0.1114 mL | 0.2228 mL | 0.5571 mL | |
| 100 mM | 0.0178 mL | 0.0891 mL | 0.1783 mL | 0.4456 mL |